Aside from a healthy host immune response, therapeutic regimens employing antibiotics now represent the primary course of treatment for most infectious diseases in developed countries. An important class of antibiotics effective against Gram-positive bacteria is lipopeptide antibiotics. Generally, lipopeptide antibiotics have either a cyclic peptide core or a cyclic depsipeptide core acylated with a lipophilic fragment. The lipophilic fragment (e.g., an unsaturated fatty acid) may vary in length and this length may affect the activity of a particular lipopeptide.
However, due to the widespread use of antibiotics, drug-resistance to these and other antibiotics is becoming an increasingly common problem all over the world for controlling several previously treatable infectious diseases. For example, infections due to Gram-positive, drug-resistant organisms, such as those due to vancomycin-resistant Enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA), are on the rise. Moreover, the leading cause of nosocomial infections (i.e., those arising in hospitals) is now due to Gram-positive cocci, and bacteria having resistance to multiple antibiotics is increasingly common.
Given the rampant rise of strains of microorganisms that are resistant to current antibiotic therapies, there is a continuing need for the development of novel antibiotics and antibiotics with novel mechanisms of action. The present invention meets such needs, and further provides other related advantages.